scholarly journals Structures and Biological Activities of Diketopiperazines from Marine Organisms: A Review

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 403
Author(s):  
Zhiqiang Song ◽  
Yage Hou ◽  
Qingrong Yang ◽  
Xinpeng Li ◽  
Shaohua Wu
Keyword(s):  
Drug Discovery ◽  
Natural Product ◽  
Biological Activities ◽  
Review Article ◽  
Membered Ring ◽  
Marine Organisms ◽  
Biological Functions ◽  
Chemical Structures ◽  
Marine Habitats ◽  
Long Time

Diketopiperazines are potential structures with extensive biological functions, which have attracted much attention of natural product researchers for a long time. These compounds possess a stable six-membered ring, which is an important pharmacophore. The marine organisms have especially been proven to be a wide source for discovering diketopiperazine derivatives. In recent years, more and more interesting bioactive diketopiperazines had been found from various marine habitats. This review article is focused on the new 2,5-diketopiperazines derived from marine organisms (sponges and microorganisms) reported from the secondary half-year of 2014 to the first half of the year of 2021. We will comment their chemical structures, biological activities and sources. The objective is to assess the merit of these compounds for further study in the field of drug discovery.

scholarly journals Sphingolipids of Asteroidea and Holothuroidea: Structures and Biological Activities

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 330
Author(s):  
Timofey V. Malyarenko ◽  
Alla A. Kicha ◽  
Valentin A. Stonik ◽  
Natalia V. Ivanchina
Keyword(s):  
Marine Invertebrates ◽  
Biological Activities ◽  
Complete Information ◽  
Structural Features ◽  
Marine Organisms ◽  
Structural Components ◽  
Chemical Structures ◽  
The Past ◽  
Complex Lipids ◽  
Complex Sphingolipids

Sphingolipids are complex lipids widespread in nature as structural components of biomembranes. Commonly, the sphingolipids of marine organisms differ from those of terrestrial animals and plants. The gangliosides are the most complex sphingolipids characteristic of vertebrates that have been found in only the Echinodermata (echinoderms) phylum of invertebrates. Sphingolipids of the representatives of the Asteroidea and Holothuroidea classes are the most studied among all echinoderms. In this review, we have summarized the data on sphingolipids of these two classes of marine invertebrates over the past two decades. Recently established structures, properties, and peculiarities of biogenesis of ceramides, cerebrosides, and gangliosides from starfishes and holothurians are discussed. The purpose of this review is to provide the most complete information on the chemical structures, structural features, and biological activities of sphingolipids of the Asteroidea and Holothuroidea classes.

Steroidal pyrazolines as a promising scaffold in drug discovery

2020 ◽  
Vol 12 (10) ◽  
pp. 949-959
Author(s):  
Ranju Bansal ◽  
Ranjit Singh
Keyword(s):  
Drug Discovery ◽  
Broad Spectrum ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Review Article ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Wide Range

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.

scholarly journals Marine natural products from sponges (Porifera) of the order Dictyoceratida (2013 to 2019); a promising source for drug discovery

RSC Advances ◽  
2020 ◽  
Vol 10 (57) ◽  
pp. 34959-34976
Author(s):  
Enas Reda Abdelaleem ◽  
Mamdouh Nabil Samy ◽  
Samar Yehia Desoukey ◽  
Miaomiao Liu ◽  
Ronald J. Quinn ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Marine Natural Products ◽  
Biological Activities ◽  
Marine Organisms ◽  
Promising Source ◽  
Secondary Natural Products

Marine organisms have been considered an interesting target for the discovery of different classes of secondary natural products with wide-ranging biological activities.

scholarly journals An Updated Review on Synthesis and Biological Activities of Thiosemicarbazide Analogs

2021 ◽  
Vol 33 (9) ◽  
pp. 1957-1975
Author(s):  
Akhalesh Kumar ◽  
Rakhi Mishra ◽  
Avijit Mazumder ◽  
Rupa Mazumder ◽  
Arun Kumar
Keyword(s):  
Drug Discovery ◽  
Review Paper ◽  
Biological Activities ◽  
Reaction Scheme ◽  
Review Article ◽  
Pharmacological Activities ◽  
Thiosemicarbazide Derivative ◽  
Synthetic Methodologies ◽  
Thiosemicarbazide Derivatives

This review paper focuses on the different synthetic methodologies that researchers have adopted to synthesize various thiosemicarbazide derivatives with different biological activities of synthesized compounds in the last 20 years. Most of the investigations available in the literature are directed to the biological activities of thiosemicarbazide derivatives with less discussion on its synthetic schemes. This review article presents various reaction scheme, which has been adopted for thiosemicarbazide derivative synthesis along with the reported pharmacological activities of synthesized analogs. The available literature in the article aims to encourage more studies on the synthesis of thiosemicarbazide derivatives, which will help for drug discovery having thiosemicarbazide nucleus.

scholarly journals An Overview of Bioactive 1,3-Oxazole-Containing Alkaloids from Marine Organisms

2021 ◽  
Vol 14 (12) ◽  
pp. 1274
Author(s):  
Jinyun Chen ◽  
Sunyan Lv ◽  
Jia Liu ◽  
Yanlei Yu ◽  
Hong Wang ◽  
...  
Keyword(s):  
Nitrogen Atom ◽  
Chemical Synthesis ◽  
Biological Activities ◽  
Structural Features ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Marine Organisms ◽  
Chemical Structures ◽  
First Time ◽  
Oxazole Derivatives

1,3-Oxazole chemicals are a unique class of five-membered monocyclic heteroarenes, containing a nitrogen atom and an oxygen. These alkaloids have attracted extensive attention from medicinal chemists and pharmacologists owing to their diverse arrays of chemical structures and biological activities, and a series of 1,3-oxazole derivatives has been developed into therapeutic agents (e.g., almoxatone, befloxatone, cabotegravir, delpazolid, fenpipalone, haloxazolam, inavolisib). A growing amount of evidence indicates that marine organisms are one of important sources of 1,3-oxazole-containing alkaloids. To improve our knowledge regarding these marine-derived substances, as many as 285 compounds are summarized in this review, which, for the first time, highlights their sources, structural features and biological properties, as well as their biosynthesis and chemical synthesis. Perspective for the future discovery of new 1,3-oxazole compounds from marine organisms is also provided.

A Recent Look into Natural Products that have Potential to Inhibit Cholinesterases and Monoamine Oxidase B: Update for 2010-2019

2020 ◽  
Vol 23 (9) ◽  
pp. 862-876
Author(s):  
Hayrettin O. Gulcan ◽  
Ilkay E. Orhan
Keyword(s):  
Natural Products ◽  
Monoamine Oxidase ◽  
Natural Product ◽  
Biological Activities ◽  
Treatment Options ◽  
Monoamine Oxidase B ◽  
Chemical Structures ◽  
Natural Agents ◽  
Natural Product Research ◽  
Multiple Receptors

With respect to the unknowns of pathophysiology of Alzheimer’s Disease (AD)-, and Parkinson’s Disease (PD)-like neurodegenerative disorders, natural product research is still one of the valid tools in order to provide alternative and/or better treatment options. At one hand, various extracts of herbals provide a combination of actions targeting multiple receptors, on the other hand, the discovery of active natural products (i.e., secondary metabolites) generally offers alternative chemical structures either ready to be employed in clinical studies or available to be utilized as important scaffolds for the design of novel agents. Regarding the importance of certain enzymes (e.g. cholinesterase and monoamine oxidase B), for the treatment of AD and PD, we have surveyed the natural product research within this area in the last decade. Particularly novel natural agents discovered within this period, concomitant to novel biological activities displayed for known natural products, are harmonized within the present study.

scholarly journals Drug Discovery Inspired by Mother Nature: Seeking Natural Biochemotypes and the Natural Assembly Rules of the Biochemome

2013 ◽  
Vol 16 (2) ◽  
pp. 331 ◽  
Author(s):  
Qiong Gu ◽  
Xin Yan ◽  
Jun Xu
Keyword(s):  
Drug Discovery ◽  
Periodic Table ◽  
Drug Targets ◽  
Biological Activities ◽  
Building Blocks ◽  
Genome Project ◽  
New Paradigm ◽  
Chemical Library ◽  
Chemical Structures ◽  
Natural Building

Purpose. The Human Genome Project is producing a new biological ‘periodic table’, which defines all genes for making macromolecules (proteins, DNA, RNA, etc) and the relations between genes and their biological functions. We now need to consider whether to initiate a biochemome project aimed at discovering biochemistry’s ‘periodic table’, which would define all molecular parts for making small molecules (natural products) and the relations between the parts and their functions to regulate genes. By understanding the Biochemome, we might be able to design biofunctional molecules based upon a set of molecular parts for drug innovation. Methods. A number of algorithms for processing chemical structures are used to systematically derive chemoyls (natural building blocks) from a database of compounds identified in Traditional Chinese Medicine (TCM). The rules to combine chemoyls for biological activities are then deduced by mining an annotated TCM structure-activity database (ATCMD). Based upon the rules and the basic chemoyls, a chemical library can be biochemically profiled, virtual synthetic routes can be planned, and lead compounds can be identified for a specific drug target. Conclusions. The Biochemome is the complete set of molecular components (chemoyls) in an organism and Biochemomics studies the rules governing their assembly and their evolution, together with the relations between the Biochemome and drug targets. This approach provides a new paradigm for drug discovery that is based on a comprehensive knowledge of the synthetic origins of biochemical diversity, and helps to direct biomimetic syntheses aimed at assembling quasi-natural product libraries for drug screening.   This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Metabolites from Marine Microorganisms, Micro, and Macroalgae: Immense Scope for Pharmacology

Marine Drugs ◽  
2019 ◽  
Vol 17 (8) ◽  
pp. 464 ◽  
Author(s):  
Barzkar ◽  
Tamadoni Jahromi ◽  
Poorsaheli ◽  
Vianello
Keyword(s):  
Clinical Trials ◽  
Natural Products ◽  
Drug Discovery ◽  
Biological Activities ◽  
Marine Organisms ◽  
Large Array ◽  
New Wave ◽  
Marine Microorganisms ◽  
Marine Metabolites ◽  
Advanced Stages

Marine organisms produce a large array of natural products with relevance in drug discovery. These compounds have biological activities such as antioxidant, antibacterial, antitumor, antivirus, anticoagulant, anti-inflammatory, antihypertensive, antidiabetic, and so forth. Consequently, several of the metabolites have made it to the advanced stages of clinical trials, and a few of them are commercially available. In this review, novel information on natural products isolated from marine microorganisms, microalgae, and macroalgae are presented. Given due research impetus, these marine metabolites might emerge as a new wave of promising drugs.

scholarly journals Natural product as a source of prodrug

2017 ◽  
Vol 12 (2) ◽  
pp. 5
Author(s):  
Jagannathan Padmavathy ◽  
Saravanan Devarajan
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Drug Design ◽  
Chemical Synthesis ◽  
Natural Product ◽  
Chemical Constituents ◽  
Living Organism ◽  
Review Article ◽  
Complex Mixtures ◽  
Chemical Variability

<p class="Abstract">The natural products are the chemical constituents that are generated from the living organism. The natural products are isolated from the plants, animals, and microorganisms which are used in drug design and drug discovery. Natural product is then modified by chemical synthesis as either total or semi-synthetic way. The natural products show various pharmacological activity which can be used for the treatment of a variety of diseases. Natural products could be regarded as a source of quantifiable and chemically pure known products and also natural products can be utilized as complex mixtures subjected to chemical variability. The present review article adds up the prodrugs from natural products as well as prodrugs developed from the natural products.</p>

scholarly journals Cheminformatics to Characterize Pharmacologically Active Natural Products

Biomolecules ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 1566 ◽  
Author(s):  
José L. Medina-Franco ◽  
Fernanda I. Saldívar-González
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Natural Product ◽  
Chemical Space ◽  
Data Sets ◽  
Fragment Analysis ◽  
Chemical Structures ◽  
Speed Up ◽  
Pharmacologically Active ◽  
Design Experiments

Natural products have a significant role in drug discovery. Natural products have distinctive chemical structures that have contributed to identifying and developing drugs for different therapeutic areas. Moreover, natural products are significant sources of inspiration or starting points to develop new therapeutic agents. Natural products such as peptides and macrocycles, and other compounds with unique features represent attractive sources to address complex diseases. Computational approaches that use chemoinformatics and molecular modeling methods contribute to speed up natural product-based drug discovery. Several research groups have recently used computational methodologies to organize data, interpret results, generate and test hypotheses, filter large chemical databases before the experimental screening, and design experiments. This review discusses a broad range of chemoinformatics applications to support natural product-based drug discovery. We emphasize profiling natural product data sets in terms of diversity; complexity; acid/base; absorption, distribution, metabolism, excretion, and toxicity (ADME/Tox) properties; and fragment analysis. Novel techniques for the visual representation of the chemical space are also discussed.

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